2. GPCR/G Protein Neuronal Signaling
  3. Adrenergic Receptor
  4. KMCA-0011

KMCA-0011 是一种口服有效的 ɑ2C 肾上腺素受体 (ɑ2C adrenoceptor) 拮抗剂 (Ki = 56.7 nM)。KMCA-0011 通过增强脑源性神经营养因子 (BDNF) 和突触可塑性来缓解抑郁行为。KMCA-0011 具有良好的代谢稳定性，包括血浆稳定性高 (120 分钟后仍保持 99.8%)。KMCA-0011 可用于抑郁症的研究。

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KMCA-0011

KMCA-0011 Chemical Structure

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规格 价格 是否有货 数量
5 mg ￥2880
3 - 5 周
10 mg ￥4640
3 - 5 周
25 mg 询价 3 - 5 周
50 mg 询价 3 - 5 周
100 mg   询价  
200 mg   询价  

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KMCA-0011 相关抗体

Top Publications Citing Use of Products

查看 Adrenergic Receptor 亚型特异性产品:

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α adrenergic receptor β adrenergic receptor

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

KMCA-0011 is an orally active ɑ2C adrenoceptor antagonist (Ki = 56.7 nM). KMCA-0011 alleviates depressive behaviors by enhancing BDNF and synaptic plasticity. KMCA-0011 displays favorable metabolic stability, including high plasma stability (99.8% after 120 min). KMCA-0011 can be used for the research of depression[1].

IC50 & Target[1]

Alpha-2C adrenergic receptor

56.7 nM (Ki)

体外研究
(In Vitro)

KMCA-0011 (Compound 11e) 对人 HEK-293 细胞中的 ɑ2C 肾上腺素受体表现出显著的高结合亲和力 (Ki = 56.7 nM)[1]。
KMCA-0011 (10 μM) 可有效抑制肾上腺素 (HY-B0447) 诱导的 ERK 磷酸化[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

KMCA-0011 相关抗体:

Western Blot Analysis[1]

Cell Line: ɑ2C Adrenoceptor cDNA-transfected HEK-293 cells
Concentration: 10 μM
Incubation Time:
Result: Induced no detectable ERK phosphorylation, indicating the absence of agonist activity.
Inhibited Epinephrine-induced ERK phosphorylation.
体内研究
(In Vivo)

KMCA-0011 (Compound 11e) (1-10 mg/kg, 口服, 每日一次, 持续一周) 在多项测试中表现出最一致的行为疗效，独特地改善了 EPM 测试中的焦虑样行为，增加了海马 BDNF 表达，并恢复了母子分离 (MS) 小鼠模型中 CORT 诱导的突触可塑性损伤[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Maternal separation (MS) mouse model in ICR mice (7 weeks)[1]
Dosage: 1, 3, 10 mg/kg
Administration: oral gavage (p.o.), daily for one week
Result: Exhibited rapid antidepressant-like effects after a single administration, accompanied by enhanced synaptic plasticity.
Markedly improved cognitive dysfunction and reduced immobility time at all tested doses.
Neither decreased distance moved nor induced hyperactivity-like side effects.
Showed the most pronounced effect at 3 mg/kg, suggesting an improvement in anhedonia.
Restored sociability at 10 mg/kg.
Specifically improved MS-induced anxiety.
Significantly elevated BDNF expression at 10 mg/kg, indicating antidepressant activity through BDNF signaling modulation.
Effectively reversed the CORT-induced LTP impairment.
分子量

397.90

Formula

C22H24ClN3O2
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

KMCA-0011 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

KMCA-0011KMCA0011KMCA 0011Adrenergic ReceptorBeta Receptorɑ2CadrenoceptorAntagonistAntidepressantMolecular dockingMaternal separation mouseInhibitorinhibitorinhibit

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目录号：
HY-179390
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